Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites.
Org Biomol Chem
; 12(41): 8132-7, 2014 Nov 07.
Article
em En
| MEDLINE
| ID: mdl-25230674
ABSTRACT
N-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub-micromolar peptidomimetic inhibitors of Plasmodium and Leishmania NMTs. High-resolution structures of these inhibitors with Plasmodium and Leishmania NMTs permit a comparative analysis of binding modes, and provide the first crystal structure evidence for a ternary NMT-Coenzyme A/myristoylated peptide product complex.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Plasmodium
/
Aciltransferases
/
Inibidores Enzimáticos
/
Peptidomiméticos
/
Leishmania
/
Antifúngicos
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article